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Bicalutamide

AEMPS

Non-steroidal antiandrogen

ATC code: L02BB03

Updated · Methodology

Indications

B

Prostate cancer

Second line

Foundation therapy in metastatic hormone-sensitive prostate cancer within maximum androgen blockade with GnRH agonists (leuprolide, goserelin) per EAU 2024. Dose 50 mg once daily. In the first 1–2 weeks after GnRH agonist start, used to prevent the testosterone flare. Monotherapy at 150 mg daily is possible in localized cancer without metastases as an alternative to androgen-deprivation therapy – with better quality of life but lower survival.

Sources

  1. Eur Urol: EAU-EANM-ESTRO-ESUR-ISUP-SIOG Guidelines on Prostate Cancer-2024 Update. Part I: Screening, Diagnosis, and Local Treatment with Curative Intent. (2024)
  2. AEMPS: Ficha técnica de Bicalutamida (2024)
  3. Cochrane Database Syst Rev: Non-steroidal antiandrogen monotherapy compared with luteinising hormone-releasing hormone agonists or surgical castration monotherapy for advanced prostate cancer. (2014)
  4. Lancet: Maximum androgen blockade in advanced prostate cancer: an overview of the randomised trials. Prostate Cancer Trialists' Collaborative Group. (2000)
  5. BJU Int: Antiandrogen monotherapy in patients with localized or locally advanced prostate cancer: final results from the bicalutamide Early Prostate Cancer programme at a median follow-up of 9.7 years. (2010)

ICD-10: C61 · ICD-11: 2C82

Marketing claims without evidence base

The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.

How to read tiers A–F
  • AStrong evidence – first or second line in international guidelines
  • BRecommended in selected cases
  • CStudy data contradict each other
  • DBenefit not proven, no documented harm
  • FDocumented harm, or risk without benefit

Mechanism of action

A competitive non-steroidal androgen receptor antagonist in target tissues (prostate, skin, hypothalamus). Unlike cyproterone acetate, it lacks progestogenic activity and does not suppress LH – testosterone remains normal or elevated. This preserves libido and physical strength in prostate cancer patients but requires combination with GnRH agonists or antagonists for full androgen blockade. CYP3A4-metabolized, half-life 6 days.

Safety

Contraindications

  • Bicalutamide hypersensitivity
  • Severe hepatic impairment
  • Use in women and children
  • Concomitant terfenadine, astemizole, cisapride (arrhythmia risk)

Serious adverse effects

  • Hepatotoxicity up to acute liver failure (FDA warning)
  • Interstitial lung disease
  • Cardiovascular events (QT prolongation, atrial fibrillation)
  • Severe anemia
  • Venous thromboembolism

Common adverse effects

  • Gynecomastia and breast tenderness (35–70% on monotherapy)
  • Hot flashes and night sweats
  • Reduced libido and erectile dysfunction
  • Fatigue
  • Weight gain

Pregnancy: can you take Bicalutamide?

Not used in women. Men on therapy must use barrier contraception to prevent fetal exposure to the partner.

Breastfeeding: can you take Bicalutamide?

Not used in women.

Calculate RID

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Practical notes

Timing and administration

Take once daily, with or without food, preferably at the same time. Before start and every 3 months, monitor liver function – severe hepatotoxicity with possible fatal outcome risk. Discontinue immediately if jaundice, nausea, abdominal pain, or loss of appetite emerges. Monitor CBC (anemia risk) and PSA (efficacy assessment).
Label mentions18 mentions

Verbatim lines from the interaction sections, in the language of the label

From this drug’s label

  • CriticalCisapride
    «Está contraindicada la administración concomitante de terfenadina, astemizol o cisaprida con»

    AEMPS, section 4.3 · Open on CIMA

  • MajorCiclosporin
    «Aunque estudios clínicos que utilizaron antipirina como un marcador de la actividad del citocromo P450 (CYP) no mostraron evidencia de una potencial interacción de fármacos con bicalutamida, la…»

    AEMPS, section 4.5 · Open on CIMA

  • Moderateantagonistas del calcioclass named in the label
    «Aunque estudios clínicos que utilizaron antipirina como un marcador de la actividad del citocromo P450 (CYP) no mostraron evidencia de una potencial interacción de fármacos con bicalutamida, la…»

    AEMPS, section 4.5 · Open on CIMA

  • Moderateanticoagulantesclass named in the label
    «Los estudios in vitro han demostrado que bicalutamida puede desplazar al anticoagulante cumarínico warfarina, de sus lugares de unión a proteínas; por tanto, se recomienda que si se inicia el…»

    AEMPS, section 4.5 · Open on CIMA

  • Moderateanticoagulantsclass named in the label
    «7. DRUG INTERACTIONS: In vitro protein binding studies have shown that bicalutamide can displace coumarin anticoagulants from binding sites. PT/INR should be closely monitored in patients…»

    FDA, section 7 · Open on DailyMed

  • ModerateKetoconazole
    «Se deberá tener precaución cuando se prescriba Eftoran con otros fármacos que puedan inhibir la oxidación del fármaco por ejemplo, cimetidina y ketoconazol. En teoría, esto podría originar un…»

    AEMPS, section 4.5 · Open on CIMA

  • ModerateWarfarin
    «Los estudios in vitro han demostrado que bicalutamida puede desplazar al anticoagulante cumarínico warfarina, de sus lugares de unión a proteínas; por tanto, se recomienda que si se inicia el…»

    AEMPS, section 4.5 · Open on CIMA

  • Amiodarone
    «Se debe valorar cuidadosamente el uso concomitante de Eftoran con medicamentos que prolongan el intervalo QT o medicamentos capaces de inducir Torsade des Pointes, tales como antiarrítmicos de clase…»

    AEMPS, section 4.5 · Open on CIMA

  • antiarrítmicosclass named in the label
    «Se debe valorar cuidadosamente el uso concomitante de Eftoran con medicamentos que prolongan el intervalo QT o medicamentos capaces de inducir Torsade des Pointes, tales como antiarrítmicos de clase…»

    AEMPS, section 4.5 · Open on CIMA

  • antipsicóticosclass named in the label
    «Se debe valorar cuidadosamente el uso concomitante de Eftoran con medicamentos que prolongan el intervalo QT o medicamentos capaces de inducir Torsade des Pointes, tales como antiarrítmicos de clase…»

    AEMPS, section 4.5 · Open on CIMA

  • Dofetilide
    «Se debe valorar cuidadosamente el uso concomitante de Eftoran con medicamentos que prolongan el intervalo QT o medicamentos capaces de inducir Torsade des Pointes, tales como antiarrítmicos de clase…»

    AEMPS, section 4.5 · Open on CIMA

  • medicamentos que prolongan el QTclass named in the label
    «Se debe valorar cuidadosamente el uso concomitante de Eftoran con medicamentos que prolongan el intervalo QT o medicamentos capaces de inducir Torsade des Pointes, tales como antiarrítmicos de clase…»

    AEMPS, section 4.5 · Open on CIMA

  • Methadone
    «Se debe valorar cuidadosamente el uso concomitante de Eftoran con medicamentos que prolongan el intervalo QT o medicamentos capaces de inducir Torsade des Pointes, tales como antiarrítmicos de clase…»

    AEMPS, section 4.5 · Open on CIMA

  • Moxifloxacin
    «Se debe valorar cuidadosamente el uso concomitante de Eftoran con medicamentos que prolongan el intervalo QT o medicamentos capaces de inducir Torsade des Pointes, tales como antiarrítmicos de clase…»

    AEMPS, section 4.5 · Open on CIMA

  • Quinidine
    «Se debe valorar cuidadosamente el uso concomitante de Eftoran con medicamentos que prolongan el intervalo QT o medicamentos capaces de inducir Torsade des Pointes, tales como antiarrítmicos de clase…»

    AEMPS, section 4.5 · Open on CIMA

  • Sotalol
    «Se debe valorar cuidadosamente el uso concomitante de Eftoran con medicamentos que prolongan el intervalo QT o medicamentos capaces de inducir Torsade des Pointes, tales como antiarrítmicos de clase…»

    AEMPS, section 4.5 · Open on CIMA

From other drugs’ labels

  • Warfarin
    «Fármacos que desplazan a los anticoagulantes de su unión a proteínas plasmáticas, con potenciación de la actividad anticoagulante: ácido etacrínico, ácido nalidíxico, antiinflamatorios no…»

    AEMPS, section 4.5 · Open on CIMA

  • Warfarin
    «CYP450 Interactions: CYP3A4 alprazolam, amiodarone, amlodipine, amprenavir, aprepitant, atorvastatin, atazanavir, bicalutamide, cilostazol, cimetidine, ciprofloxacin, clarithromycin, conivaptan…»

    FDA, section 7 · Open on DailyMed

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Frequently asked

What is Bicalutamide used for?

Bicalutamide is evaluated for the following indications with varying evidence strength: Prostate cancer (evidence tier B), Athletic endurance (evidence tier F). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Bicalutamide?

Common side effects of Bicalutamide (≥ 1 in 100): Gynecomastia and breast tenderness (35–70% on monotherapy), Hot flashes and night sweats, Reduced libido and erectile dysfunction, Fatigue, Weight gain. See the Safety section for uncommon and serious reactions.

Is Bicalutamide safe during pregnancy?

Not used in women. Men on therapy must use barrier contraception to prevent fetal exposure to the partner.

Is Bicalutamide compatible with breastfeeding?

Not used in women.

Who should not take Bicalutamide?

Bicalutamide is contraindicated in: Bicalutamide hypersensitivity; Severe hepatic impairment; Use in women and children; Concomitant terfenadine, astemizole, cisapride (arrhythmia risk). Full list in the Safety section.

Official sources

Direct links to regulator labels. Open in a new tab.

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